PE20151982A1 - BENZHIMIDAZOLONE DERIVATIVES AS BROMODOMINIUM INHIBITORS - Google Patents
BENZHIMIDAZOLONE DERIVATIVES AS BROMODOMINIUM INHIBITORSInfo
- Publication number
- PE20151982A1 PE20151982A1 PE2015002057A PE2015002057A PE20151982A1 PE 20151982 A1 PE20151982 A1 PE 20151982A1 PE 2015002057 A PE2015002057 A PE 2015002057A PE 2015002057 A PE2015002057 A PE 2015002057A PE 20151982 A1 PE20151982 A1 PE 20151982A1
- Authority
- PE
- Peru
- Prior art keywords
- derivatives
- bromodominium
- benzhimidazolone
- inhibitors
- compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Abstract
Se refiere al desarrollo de derivados de bencimidazolona de formula (I), donde R1a, R1b, R2a, R2b, R3, y X son aqui descritos. Estos compuestos son moduladores de la actividad de una proteina que contiene bromodominio, incluyendo la proteina 4 que contiene bromodominio (BRD4), por lo que son utiles en el tratamiento de cancer, diabetes, obesidad, entre otros. Tambien, se incluye las composiciones y formulaciones que contienen tales compuestos, y metodos de uso y fabricacion de tales compuestosIt refers to the development of benzimidazolone derivatives of formula (I), where R1a, R1b, R2a, R2b, R3, and X are described herein. These compounds are modulators of the activity of a protein that contains bromodomain, including protein 4 that contains bromodomain (BRD4), for which they are useful in the treatment of cancer, diabetes, obesity, among others. Also included are compositions and formulations containing such compounds, and methods of use and manufacture of such compounds.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361805995P | 2013-03-28 | 2013-03-28 | |
| US201361860230P | 2013-07-30 | 2013-07-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151982A1 true PE20151982A1 (en) | 2016-01-28 |
Family
ID=50897885
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002057A PE20151982A1 (en) | 2013-03-28 | 2014-03-27 | BENZHIMIDAZOLONE DERIVATIVES AS BROMODOMINIUM INHIBITORS |
Country Status (35)
| Country | Link |
|---|---|
| US (2) | US20160031868A1 (en) |
| EP (1) | EP2978759B1 (en) |
| JP (1) | JP6339175B2 (en) |
| KR (1) | KR101847698B1 (en) |
| CN (1) | CN105102453B (en) |
| AP (1) | AP2015008741A0 (en) |
| AU (1) | AU2014241152B2 (en) |
| BR (1) | BR112015024078A2 (en) |
| CA (1) | CA2907502C (en) |
| CL (1) | CL2015002871A1 (en) |
| CR (1) | CR20150515A (en) |
| CY (1) | CY1119165T1 (en) |
| DK (1) | DK2978759T3 (en) |
| EA (1) | EA029497B1 (en) |
| ES (1) | ES2626397T3 (en) |
| HK (1) | HK1220692A1 (en) |
| HR (1) | HRP20170750T1 (en) |
| HU (1) | HUE034772T2 (en) |
| IL (1) | IL241186A0 (en) |
| LT (1) | LT2978759T (en) |
| MD (1) | MD4531C1 (en) |
| MX (1) | MX2015013798A (en) |
| MY (1) | MY176634A (en) |
| NZ (1) | NZ711586A (en) |
| PE (1) | PE20151982A1 (en) |
| PH (1) | PH12015502246A1 (en) |
| PL (1) | PL2978759T3 (en) |
| PT (1) | PT2978759T (en) |
| RS (1) | RS56050B1 (en) |
| SG (1) | SG11201507926RA (en) |
| SI (1) | SI2978759T1 (en) |
| TW (1) | TWI530499B (en) |
| UY (1) | UY35516A (en) |
| WO (1) | WO2014160873A1 (en) |
| ZA (1) | ZA201506356B (en) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101641339B (en) | 2007-02-01 | 2013-07-17 | 雷斯韦洛吉克斯公司 | Compounds for the prevention and treatment of cardiovascular diseases |
| MX2021012876A (en) | 2009-03-18 | 2022-06-23 | Resverlogix Corp | Novel anti-inflammatory agents. |
| PT2773354T (en) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Oral immediate release formulations for substituted quinazolinones |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| BR112015022942B1 (en) | 2013-03-15 | 2022-02-22 | Incyte Holdings Corporation | Tricyclic heterocycle compounds, method for inhibiting bet protein in vitro and pharmaceutical composition comprising said compounds |
| AU2014284616B2 (en) | 2013-06-21 | 2019-02-28 | Zenith Epigenetics Ltd. | Novel bicyclic bromodomain inhibitors |
| CA2915622C (en) * | 2013-06-21 | 2020-08-18 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| JP2016523964A (en) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Tricyclic heterocycles as BET protein inhibitors |
| CA2919948C (en) | 2013-07-31 | 2020-07-21 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| NZ763740A (en) | 2014-04-23 | 2023-06-30 | Incyte Holdings Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins |
| JP6599979B2 (en) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Tricyclic heterocyclic compounds for use as BET protein inhibitors |
| WO2016061144A1 (en) | 2014-10-14 | 2016-04-21 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
| CA2966303A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| EP3227281A4 (en) | 2014-12-01 | 2018-05-30 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| CA2966449A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| JP2017538721A (en) | 2014-12-17 | 2017-12-28 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | Bromodomain inhibitors |
| US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| EP3397640B1 (en) | 2015-12-29 | 2021-08-04 | INSERM - Institut National de la Santé et de la Recherche Médicale | Xanthine derivative inhibitors of bet proteins |
| FI3472157T3 (en) | 2016-06-20 | 2023-06-01 | Incyte Corp | Crystalline solid forms of a bet inhibitor |
| US20180179191A1 (en) * | 2016-11-22 | 2018-06-28 | Gilead Sciences, Inc. | Synthesis of a compound that modulates the activity of bromodomain-containing proteins |
| JP7254075B2 (en) | 2017-11-06 | 2023-04-07 | サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック | Xanthine derivatives and their use as inhibitors of the bromodomain of BET proteins |
| JP2021506903A (en) | 2017-12-20 | 2021-02-22 | 貝達薬業股▲ふん▼有限公司Ｂｅｔｔａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｃｏ．，Ｌｔｄ | Compounds and compositions that are bromodomain protein inhibitors |
| CN113365699A (en) * | 2019-02-02 | 2021-09-07 | 石药集团中奇制药技术（石家庄）有限公司 | Target ubiquitination degradation BRD4 protein compound and preparation method and application thereof |
| CN109912584B (en) * | 2019-03-22 | 2021-08-13 | 中国药科大学 | BRD4 protein inhibitor with anti-tumor activity and preparation method and application thereof |
| KR20220077138A (en) | 2019-09-30 | 2022-06-08 | 쿄와 기린 가부시키가이샤 | BET disintegrant |
| AU2021276673A1 (en) * | 2020-05-21 | 2022-12-22 | Stemsynergy Therapeutics, Inc. | Notch inhibitors and uses thereof |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) * | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) * | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) * | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) * | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| EP1620413A2 (en) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| AU2008287421A1 (en) | 2007-08-10 | 2009-02-19 | Glaxosmithkline Llc | Nitrogen containing bicyclic chemical entities for treating viral infections |
| US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CA2828456C (en) | 2011-03-03 | 2021-05-04 | Zalicus Pharmaceuticals Ltd. | N-benzl-amino-carboxamide inhibitors of the sodium channel |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| AU2014284616B2 (en) * | 2013-06-21 | 2019-02-28 | Zenith Epigenetics Ltd. | Novel bicyclic bromodomain inhibitors |
-
2014
- 2014-03-26 TW TW103111238A patent/TWI530499B/en not_active IP Right Cessation
- 2014-03-27 AP AP2015008741A patent/AP2015008741A0/en unknown
- 2014-03-27 ES ES14729114.0T patent/ES2626397T3/en active Active
- 2014-03-27 PL PL14729114T patent/PL2978759T3/en unknown
- 2014-03-27 WO PCT/US2014/032031 patent/WO2014160873A1/en active Application Filing
- 2014-03-27 US US14/774,019 patent/US20160031868A1/en not_active Abandoned
- 2014-03-27 EP EP14729114.0A patent/EP2978759B1/en active Active
- 2014-03-27 RS RS20170569A patent/RS56050B1/en unknown
- 2014-03-27 MD MDA20150104A patent/MD4531C1/en not_active IP Right Cessation
- 2014-03-27 PT PT147291140T patent/PT2978759T/en unknown
- 2014-03-27 AU AU2014241152A patent/AU2014241152B2/en not_active Ceased
- 2014-03-27 DK DK14729114.0T patent/DK2978759T3/en active
- 2014-03-27 MX MX2015013798A patent/MX2015013798A/en unknown
- 2014-03-27 CA CA2907502A patent/CA2907502C/en not_active Expired - Fee Related
- 2014-03-27 KR KR1020157030708A patent/KR101847698B1/en active IP Right Grant
- 2014-03-27 CN CN201480018645.6A patent/CN105102453B/en active Active
- 2014-03-27 SG SG11201507926RA patent/SG11201507926RA/en unknown
- 2014-03-27 HU HUE14729114A patent/HUE034772T2/en unknown
- 2014-03-27 MY MYPI2015002440A patent/MY176634A/en unknown
- 2014-03-27 NZ NZ711586A patent/NZ711586A/en not_active IP Right Cessation
- 2014-03-27 US US14/227,736 patent/US9255089B2/en active Active
- 2014-03-27 JP JP2016505567A patent/JP6339175B2/en not_active Expired - Fee Related
- 2014-03-27 BR BR112015024078A patent/BR112015024078A2/en not_active Application Discontinuation
- 2014-03-27 PE PE2015002057A patent/PE20151982A1/en not_active Application Discontinuation
- 2014-03-27 EA EA201591455A patent/EA029497B1/en not_active IP Right Cessation
- 2014-03-27 LT LTEP14729114.0T patent/LT2978759T/en unknown
- 2014-03-27 SI SI201430191A patent/SI2978759T1/en unknown
- 2014-03-28 UY UY0001035516A patent/UY35516A/en not_active Application Discontinuation
-
2015
- 2015-08-31 ZA ZA2015/06356A patent/ZA201506356B/en unknown
- 2015-09-06 IL IL241186A patent/IL241186A0/en unknown
- 2015-09-24 PH PH12015502246A patent/PH12015502246A1/en unknown
- 2015-09-25 CL CL2015002871A patent/CL2015002871A1/en unknown
- 2015-10-02 CR CR20150515A patent/CR20150515A/en unknown
-
2016
- 2016-07-25 HK HK16108876.4A patent/HK1220692A1/en unknown
-
2017
- 2017-05-19 HR HRP20170750TT patent/HRP20170750T1/en unknown
- 2017-06-13 CY CY20171100624T patent/CY1119165T1/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |